Home GPCR & G Protein GPR inhibitor PH-064

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PH-064 GPR inhibitor

Cat.No.S3451

PH-064 (BIM-46187) is a novel imidazo-pyrazine derivative that inhibits the heterotrimeric G-protein complex effectively. This compound inhibits heterotrimeric G-protein signalling in GPCRsthat mediate cyclic AMP generation (GAs), calcium release (GAq), cancer cell invasion by Wnt-2 frizzled receptors, and high-affinity neurotensin receptors (GAo/i and GAq).
PH-064 GPR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 795.11

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S345101 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.9%
99.9

Chemical Information, Storage & Stability

Molecular Weight 795.11 Formula

C44H58N8O2S2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 892546-37-1 -- Storage of Stock Solutions

Synonyms BIM-46187 Smiles NC(CSSCC(N)C(=O)N1CC[N]2C=C(N=C2C1CC3CCCCC3)C4=CC=CC=C4)C(=O)N5CC[N]6C=C(N=C6C5CC7CCCCC7)C8=CC=CC=C8

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (125.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Gα12/13 [1]
Gαq/11 [1]
Gα0 [3]
(BRET Measurements)
0.0043 nM
Gαi1 [3]
(BRET Measurements)
0.0047 nM
References

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